Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)
Sign Up to like & getrecommendations! Published in 2021 at "Mendeleev Communications"
DOI: 10.1016/j.mencom.2021.07.016
Abstract: Abstract Rare cis-configured 2,4-disubstituted 1-alkylpyridines were envisioned as ligands for trace amine associated receptor 1 (TAAR1). They were synthesized in diastereomerically pure form with the decarboxylative Castagnoli–Cushman reac-tion followed by two reduction events. Despite showing… read more here.
Keywords: cis configured; rare cis; trace amine; taar1 ... See more keywords
Molecular basis of human trace amine-associated receptor 1 activation
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DOI: 10.1038/s41467-023-44601-4
Abstract: hTA1 is a drug target for several neuropsychiatric disorders. Using cryo-EM and pharmacological assays, the authors illuminate hTA1’s similarity to neurotransmitter receptors and discover that the antipsychotic asenapine potently activates the receptor. The human trace… read more here.
Keywords: receptor; human trace; pharmacology; amine associated ... See more keywords
Evolution of Brain-Expressed Biogenic Amine Receptors into Olfactory Trace Amine-Associated Receptors
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DOI: 10.1093/molbev/msac006
Abstract: Abstract The family of trace amine-associated receptors (TAARs) is distantly related to G protein-coupled biogenic aminergic receptors. TAARs are found in the brain as well as in the olfactory epithelium where they detect biogenic amines.… read more here.
Keywords: associated receptors; brain; trace amine; amine associated ... See more keywords
A partial trace amine‐associated receptor 1 agonist exhibits properties consistent with a methamphetamine substitution treatment
Sign Up to like & getrecommendations! Published in 2017 at "Addiction Biology"
DOI: 10.1111/adb.12410
Abstract: Recent evidence suggests that the trace amine‐associated receptor 1 (TAAR1) plays a pivotal role in the regulation of dopamine (DA) transmission and psychostimulant action. Several selective TAAR1 agonists have previously shown efficacy in models of… read more here.
Keywords: taar1; trace amine; associated receptor; amine associated ... See more keywords
Vasoconstrictor Effects of Trace Amine-Associated Receptor Agonists in the Isolated Perfused Rat Kidney
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DOI: 10.1159/000540429
Abstract: Abstract Introduction: Endogenous trace amines such as tryptamine and 3-iodothyronamine (T1AM) are present in mammalian tissues at very low concentrations. They produce their actions by activating surface G protein-coupled receptors known as trace amine-associated receptors… read more here.
Keywords: perfused rat; isolated perfused; amine associated; trace amine ... See more keywords
Trace Amine-Associated Receptors as Novel Therapeutic Targets for Immunomodulatory Disorders
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DOI: 10.3389/fphar.2018.00680
Abstract: Trace amines and their receptors (trace amine-associated receptors; TAARs) are an emerging pharmacological target for the treatment of human disorders. While most studies have focused on their therapeutic potential for neurologic and psychiatric disorders, TAARs… read more here.
Keywords: immunomodulatory disorders; associated receptors; trace amine; amine ... See more keywords
Deregulation of Trace Amine-Associated Receptors (TAAR) Expression and Signaling Mode in Melanoma
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12010114
Abstract: Trace amine-associated receptors (TAARs) interact with amine compounds called “trace amines” which are present in tissues at low concentrations. Recently, TAARs expression in neoplastic tumors was reported. In this study, TAARs expression was analyzed in… read more here.
Keywords: melanoma; associated receptors; expression; trace amine ... See more keywords